ALEXIS Biochemicals: Lavendustin B

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ALX-270-316

Revised 12-Jan-07

Compound 56
SYNONYMS	4-[(3-Bromophenyl)amino]-6,7-diethoxyquinazoline
PRODUCT LINE	Signal Transduction
PRODUCT CATEGORY	EGFR Kinase Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-270-316-C500		500 µg	135.00 USD

Product Specification

FORMULA:	C₁₈H₁₈BrN₃O₂
MW:	388.3
PURITY:	≥97% (HPLC)
APPEARANCE:	White to off-white powder.
SOLUBILITY:	Soluble in DMSO.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
HANDLING:	Protect from light.
HAZARD:	MAY BE MUTAGENIC. HARMFUL.

Product Description

Potent and specific inhibitor of the tyrosine kinase activity of the epidermal growth factor receptor (EGFR) (IC₅₀=6pM).

Product Specific Literature References

Tyrosine kinase inhibitors. 8. An unusually steep structure-activity relationship for analogues of 4-(3-bromoanilino)-6,7-dimethoxyquinazoline (PD 153035), a potent inhibitor of the epidermal growth factor receptor: A.J. Bridges, et al.; J. Med. Chem. 39, 267 (1996) Abstract

Further Categories Containing This Product:

Tyrosine Kinase Inhibitors

ALX-350-009

Revised 03-Apr-08

Daidzein
SYNONYMS	4',7-Dihydroxyisoflavone
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Natural Products - Protein Kinase Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-350-009-M010		10 mg	20.00 USD
ALX-350-009-M025		25 mg	40.00 USD
ALX-350-009-M050		50 mg	60.00 USD

Product Specification

FORMULA:	C₁₅H₁₀O₄
MW:	254.2
CAS NUMBER:	486-66-8
MERCK INDEX:	14: 2801
RTECS:	DJ3100040
SOURCE/HOST:	Synthetic.
PURITY:	≥98%
APPEARANCE:	White to off-white solid.
SOLUBILITY:	Soluble in DMSO; slightly soluble in 100% ethanol; insoluble in water.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
HAZARD:	IRRITANT.

Product Description

Inactive analog of the tyrosine kinase inhibitor genistein (Prod. No. ALX-350-006). Shows anti-inflammatory effect.

Product Specific Literature References

Genistein, a specific inhibitor of tyrosine-specific protein kinases: T. Akiyama, et al.; J. Biol. Chem. 262, 5592 (1987) Abstract; Full Text
Role of tyrosine kinases in IgE-mediated signal transduction in human lung mast cells and basophils: S.E. Lavens, et al.; Am. J. Respir. Cell. Mol. Biol. 7, 637 (1992) Abstract
Tyrosine kinase inhibitors block calcium channel currents in vascular smooth muscle cells: S. Wijetunge, et al.; BBRC 189, 1620 (1992) Abstract
Genistein and daidzein, and their ß-glycoside conjugates: anti-tumor isoflavones in soybean foods from American and Asian diets: L. Coward, et al.; J. Agric. Food Chem. 41, 1961 (1993)
Stimulation of pS2 expression by diet-derived compounds: N. Sathyamoorthy, et al.; Cancer Res. 54, 957 (1994) Abstract
Daidzein inhibits insulin- or insulin-like growth factor-1-mediated signaling in cell cycle progression of Swiss 3T3 cells: K. Higashi and H. Ogawara; Biochim. Biophys. Acta 1221, 29 (1994) Abstract
Decreased circulating levels of tumor necrosis factor-alpha in postmenopausal women during consumption of soy-containing isoflavones: Y. Huang, et al.; J. Clin. Endocrinol. Metab. 90, 3956 (2005) Abstract
Gut bacterial metabolism of the soy isoflavone daidzein: exploring the relevance to human health: C. Atkinson, et al.; Exp. Biol. Med. (Maywood) 230, 155 (2005), Review Abstract
Clinical review: a critical evaluation of the role of soy protein and isoflavone supplementation in the control of plasma cholesterol concentrations: A. Dewell, et al.; J. Clin. Endocrinol. Metab. 91, 772 (2006), Review Abstract
Phytoestrogens and lipoproteins in women: C.N. Bairey Merz, et al.; J. Clin. Endocrinol. Metab. 91, 2209 (2006) Abstract

Further Categories Containing This Product:

Natural Products - Anti-inflammatory Agents • Tyrosine Kinase Inhibitors • Active Substances from Fruit and Vegetables • Flavonoids/Related Products

ALX-270-181

Revised 28-Jul-08

Damnacanthal
SYNONYMS	3-Hydroxy-1-methoxyanthraquinone-2-aldehyde
PRODUCT LINE	Immunology
PRODUCT CATEGORY	Kinases in T Cell Signal Transduction/Related Products

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-270-181-M001		1 mg	165.00 USD

Product Specification

FORMULA:	C₁₆H₁₀O₅
MW:	282.3
CAS NUMBER:	477-84-9
PURITY:	≥95% (HPLC)
APPEARANCE:	Yellow to orange solid.
SOLUBILITY:	10mg/ml soluble in DMSO.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
HANDLING:	Protect from light.

Product Description

Potent and selective inhibitor of p56^lcktyrosine kinase activity. Inhibition of p56^lckby damnacanthal appears to be reversible, not time-dependent and not significantly affected by the presence of sulfhydryl reagents.

Product Specific Literature References

S. Nonomura; J. Pharm. Soc. Jpn. 75, 219 (1955)
N.R. Ayyangar, et al.; Tetrahedron 6, 331 (1959)
Effects of three compounds extracted from Morinda lucida on Plasmodium falciparum: K.Koumaglo, et al.; Planta Medica 58, 533 (1992) Abstract
Induction of normal phenotypes in ras-transformed cells by damnacanthal from Morinda citrifolia: T. Hiramatsu, et al.; Cancer Lett. 73, 161 (1993) Abstract
Damnacanthal is a highly potent, selective inhibitor of p56lck tyrosine kinase activity: C.R. Faltynek, et al.; Biochemistry 34, 12404 (1995) Abstract

Further Categories Containing This Product:

Src Family Kinases/Related Products • Tyrosine Kinase Inhibitors

ALX-270-281

Revised 28-Sep-06

Daphnetin
SYNONYMS	7,8-Dihydroxycoumarin
PRODUCT LINE	Signal Transduction
PRODUCT CATEGORY	EGFR Kinase Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-270-281-M005		5 mg	25.00 USD
ALX-270-281-M025		25 mg	95.00 USD

Product Specification

FORMULA:	C₉H₆O₄
MW:	178.1
CAS NUMBER:	486-35-1
RTECS:	GN6382600
PURITY:	≥97%
APPEARANCE:	White to rose powder.
SOLUBILITY:	Soluble in 100% ethanol, methanol or dimethyl formamide.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	+20°C

Product Description

Inhibitor of protein kinases. EGF receptor tyrosine kinase (IC₅₀=7.87µM), PKA (IC₅₀=9.33µM), PKC (IC₅₀=25.01µM). Antioxidant. Antimalarial agent.

Product Specific Literature References

Daphnetin: a novel antimalarial agent with in vitro and in vivo activity: Y.Z. Yang, et al.; Am. J. Trop. Med. Hyg. 46, 15 (1992) Abstract
Daphnetin, one of coumarin derivatives, is a protein kinase inhibitor: E.B. Yang, et al.; BBRC 260, 682 (1999) Abstract

Further Categories Containing This Product:

PKA Inhibitors • Malaria/Related Products • Tyrosine Kinase Inhibitors • Antioxidants, Flavonoids & Free Radical Scavengers Other Products

ALX-270-364

Revised 03-Mar-05

3-(3,5-Di-tert-butyl-4-hydroxybenzylidenyl)indolin-2-one
PRODUCT LINE	Signal Transduction
PRODUCT CATEGORY	Tyrosine Kinase Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-270-364-M001		1 mg	50.00 USD
ALX-270-364-M005		5 mg	200.00 USD

Product Specification

FORMULA:	C₂₃H₂₇NO₂
MW:	349.5
CAS NUMBER:	40526-64-5
SOURCE/HOST:	Synthetic.
PURITY:	≥97% (¹H-NMR, HPLC)
APPEARANCE:	Yellow crystals.
SOLUBILITY:	Soluble in DMSO (35mg/ml) or methanol (2.5mg/ml). Sparingly soluble in aqueous buffers (25µg/ml).
SHIPPING:	AMBIENT
LONG TERM STORAGE:	+4°C
USE/STABILITY:	Stable as a powder for at least 2 years when stored at +4°C in the dark. Stock solutions made in DMSO should be stored in the dark and used within one month.
HANDLING:	Protect from light. Keep cool and dry.
IDENTITY:	Identity determined by ¹H-NMR, ¹³C-NMR, IR, ESI-MS and UV.

Product Description

Receptor tyrosine kinase (RTK) inhibitor. Inhibits FLK-1 RTK (IC₅₀~8µM) and EGF RTK. Consists of the E- and Z-isomers [1].

Product Specific Literature References

[1] Synthesis and biological evaluations of 3-substituted indolin-2-ones: a novel class of tyrosine kinase inhibitors that exhibit selectivity toward particular receptor tyrosine kinases: L. Sun, et al.; J. Med. Chem. 41, 2588 (1998) Abstract

ALX-380-110

Revised 03-Apr-08

17-DMAG
SYNONYMS	17-[2-(Dimethylamino)ethyl]amino-17-desmethoxygeldanamycin NSC 707545
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Antibiotics for Angiogenesis Research

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-380-110-C100		100 µg	50.00 USD
ALX-380-110-M001		1 mg	150.00 USD

Product Specification

FORMULA:	C₃₂H₄₈N₄O₈
MW:	616.8
CAS NUMBER:	150270-08-9
SOURCE/HOST:	Semisynthetic from geldanamycin (Prod. No. ALX-380-054).
PURITY:	≥99%
APPEARANCE:	Purple to black powder.
SOLUBILITY:	Soluble in water, 100% ethanol (10mg/ml) or DMSO (>25mg/ml).
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
HANDLING:	Protect from light.

Product Description

Less toxic, more potent synthetic derivative of geldanamycin. Inhibitor of angiogenesis. Inhibitor of heat shock protein 90 (HSP90). Inducer of apoptosis with higher antitumor activity than 17-AAG (Prod. No. ALX-380-091).

Product Specific Literature References

Pharmacokinetics, tissue distribution, and metabolism of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin (NSC 707545) in CD2F1 mice and Fischer 344 rats: M.J. Egorin, et al.; Cancer Chemother. Pharmacol. 49, 7 (2002) Abstract
Biliary excretion of 17-(allylamino)-17-demethoxygeldanamycin (NSC 330507) and metabolites by Fischer 344 rats: S.M. Musser, et al.; Cancer Chemother. Pharmacol. 52, 139 (2003) Abstract
Crystal structure and molecular modeling of 17-DMAG in complex with human Hsp90: J.M. Jez, et al.; Chem. Biol. 10, 361 (2003) Abstract
Synthesis and biological activities of novel 17-aminogeldanamycin derivatives: Z.Q. Tian, et al.; Bioorg. Med. Chem. 12, 5317 (2004) Abstract
Antiangiogenic properties of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin: an orally bioavailable heat shock protein 90 modulator: G. Kaur, et al.; Clin. Cancer Res. 10, 4813 (2004) Abstract
Enhanced tumor cell radiosensitivity and abrogation of G2 and S phase arrest by the Hsp90 inhibitor 17-(Dimethylaminoethylamino)-17-demethoxygeldanamycin: E.E. Bull, et al.; Clin. Cancer Res. 10, 8077 (2004) Abstract
ErbB3 expression predicts tumor cell radiosensitization induced by Hsp90 inhibition: H. Dote, et al.; Cancer Res. 65, 6967 (2005) Abstract
In vivo antitumor efficacy of 17-DMAG (17-dimethylaminoethylamino-17-demethoxygeldanamycin hydrochloride), a water-soluble geldanamycin derivative: M. Hollingshead, et al.; Cancer Chemother. Pharmacol. 56, 115 (2005) Abstract
Comparison of 17-dimethylaminoethylamino-17-demethoxy-geldanamycin (17DMAG) and 17-allylamino-17-demethoxygeldanamycin (17AAG) in vitro: effects on Hsp90 and client proteins in melanoma models: V. Smith, et al.; Cancer Chemother. Pharmacol. 56, 126 (2005) Abstract
Preclinical toxicity of a geldanamycin analog, 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin (17-DMAG), in rats and dogs: potential clinical relevance: E.R. Glaze, et al.; Cancer Chemother. Pharmacol. 56, 637 (2005) Abstract
17-Allyamino-17-demethoxygeldanamycin and 17-NN-dimethyl ethylene diamine-geldanamycin have cytotoxic activity against multiple gynecologic cancer cell types: D.R. Gossett, et al.; Gynecol. Oncol. 96, 381 (2005) Abstract
Structure-based design of 7-carbamate analogs of geldanamycin: G. Rastelli, et al.; Biooorg. Med. Chem. Lett. 15, 5016 (2005) Abstract
Generation of a novel anti-geldanamycin antibody: E. Barzilay, et al.; BBRC 330, 561 (2005) Abstract
Determination of the heat shock protein 90 inhibitor 17-dimethylaminoethylamino-17-demethoxygeldanamycin in plasma by liquid chromatography-electrospray mass spectrometry: K. Hwang, et al.; J. Chromatogr. B Analyt. Technol. Biomed. Life Sci. 830, 35 (2006) Abstract

Related Products

ALX-380-054	Geldanamycin
ALX-380-091	17-AAG

Further Categories Containing This Product:

Antibiotics - Apoptosis Inducers & Inhibitors • Antitumor Agents (Enzyme Inhibitors) • Tyrosine Kinase Inhibitors • Antitumor Antibiotics • HSP90/HtpG/Related Products

ALX-350-057

Revised 20-Feb-08

Emodin
SYNONYMS	6-Methyl-1,3,8-trihydroxyanthraquinone
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Natural Products - Protein Kinase Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-350-057-M025		25 mg	45.00 USD

Product Specification

FORMULA:	C₁₅H₁₀O₅
MW:	270.2
CAS NUMBER:	518-82-1
MERCK INDEX:	14: 3561
RTECS:	CB7920600
SOURCE/HOST:	Isolated from Frangula bark.
PURITY:	≥96% (HPLC)
APPEARANCE:	Orange to red solid.
SOLUBILITY:	Soluble in DMSO, 100% ethanol or 1N dilute aqueous ammonia; insoluble in water.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	+4°C
HAZARD:	IRRITANT.

Product Description

Inhibitor of p56^lck tyrosine kinase. Has mutagenic and genotoxic effects, mainly in bacterial systems. Anticancer agent. Exhibits anti-proliferative effects in various cancer cell lines by efficient induction of apoptosis. Has inhibitory effects on angiogenic and metastasis regulatory processes. Anti-inflammatory compound. Suppresses NF-κB activation.

Product Specific Literature References

Emodin, a protein tyrosine kinase inhibitor from Polygonum cuspidatum: H. Jayasuriya, et al.; J. Nat. Prod. 55, 696 (1992) Abstract
Selective inhibition of the growth of ras-transformed human bronchial epithelial cells by emodin, a protein-tyrosine kinase inhibitor: T.C.K. Chan, et al.; BBRC 193, 1152 (1993) Abstract
Molecular mechanism of emodin action: transition from laxative ingredient to an antitumor agent: G. Srinivas, et al.; Med. Res. Rev. 27, 591 (2007), (Review) Abstract

Further Categories Containing This Product:

Tyrosine Kinase Inhibitors • NF-kB Pathway Inhibitors • Kinases in T Cell Signal Transduction/Related Products • Src Family Kinases/Related Products • Natural Products - Anti-inflammatory Agents • Natural Products - NF-kB Pathway Inhibitors • Natural Products - Antitumor Reagents • Natural Products - Apoptosis Inducers & Inhibitors • Other Toxins

ALX-270-098

Revised 16-Nov-06

Erbstatin analog
SYNONYMS	Methyl 2,5-dihydroxycinnamate
PRODUCT LINE	Signal Transduction
PRODUCT CATEGORY	EGFR Kinase Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-270-098-M005		5 mg	55.00 USD

Product Specification

FORMULA:	C₁₀H₁₀O₄
MW:	194.2
CAS NUMBER:	63177-57-1
PURITY:	≥98% (HPLC)
APPEARANCE:	Off-white to light brown crystalline solid.
SOLUBILITY:	Soluble in methanol, DMSO or dilute aqueous base.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	+4°C
HANDLING:	Protect from light.
HAZARD:	TOXIC.

Product Description

Inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase. Considerably longer half-life in aqueous solution than erbstatin itself. Induces apoptosis.

Product Specific Literature References

Inhibition of epidermal growth factor-induced DNA synthesis by tyrosine kinase inhibitors: K. Umezawa, et al.; FEBS Lett. 260, 198 (1990) Abstract
Inhibition of epidermal growth factor receptor functions by tyrosine kinase inhibitors in NIH3T3 cells: K. Umezawa, et al.; FEBS Lett. 314, 289 (1992) Abstract
Induction of mouse thymocyte apoptosis by inhibitors of tyrosine kinases is associated with dephosphorylation of nuclear proteins: Y. Azuma, et al.; Cell Immunol. 152, 271 (1993) Abstract
Inhibition of Abelson oncogene function by erbstatin analogues: M. Kawada, et al.; Drugs Exp. Clin. Res. 19, 235 (1993) Abstract

Further Categories Containing This Product:

Tyrosine Kinase Inhibitors • Apoptosis Inducers & Inhibitors Other Products

ALX-380-054

Revised 18-Jun-08

Geldanamycin
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Antibiotics - Protein Kinase Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-380-054-C100		100 µg	28.00 USD
ALX-380-054-C500		500 µg	50.00 USD
ALX-380-054-M001		1 mg	75.00 USD
ALX-380-054-M005		5 mg	300.00 USD

Product Specification

FORMULA:	C₂₉H₄₀N₂O₉
MW:	560.6
CAS NUMBER:	30562-34-6
RTECS:	LX8920000
SOURCE/HOST:	Isolated from Streptomyces hygroscopicus.
PURITY:	≥96%
APPEARANCE:	Yellow solid.
SOLUBILITY:	Slightly soluble in methanol, chloroform or DMSO; insoluble in water.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
HANDLING:	Protect from light.

Product Description

Potent antitumor antibiotic. Inhibitor of pp60^src tyrosine kinase and of c-myc gene expression in murine lymphoblastoma cells. Inhibits the transforming activity of abl, erbB, fps, src, and yes. Binds specifically to heat shock protein 90 (HSP90) and to its endoplasmic reticulum homolog GP96 (GRP94). Capable of destabilizing several oncogene and proto-oncogene products. Potent inhibitor of the nuclear hormone receptor family. Protects against α-synuclein toxicity to dopaminergic neurons in Drosophila. Destabilizes mutant p53 protein from a number of breast, leukemic, and prostate cell lines. Inhibits basal and hypoxia-induced expression of c-Jun (IC₅₀=75nM) and abolishes hypoxia-induced increase in c-Jun N-terminal kinase (JNK) activity. Inhibits telomerase activity through inhibition of HSP90, a chaperone required for the assembly and activation of telomerase in human cells. ~10-fold more potent than herbimycin A (Prod. No. ALX-350-029)

Product Specific Literature References

Geldanamycin, a new antibiotic: C. DeBoer, et al.; J. Antibiot. 23, 442 (1970) Abstract
Phenotypic change from transformed to normal induced by benzoquinonoid ansamycins accompanies inactivation of p60src in rat kidney cells in